US6022876AExpiredUtility
L-β-dioxolane uridine analogs and methods for treating and preventing Epstein-Barr virus infections
Est. expiryNov 15, 2016(expired)· nominal 20-yr term from priority
A61P 35/00A61P 37/00A61P 31/12A61P 31/18A61P 31/22C07D 405/04C07D 473/00
63
PatentIndex Score
14
Cited by
36
References
42
Claims
Abstract
The present invention relates to the discovery that certain beta -L-dioxolane nucleoside analogs which contain a uracil base, and preferably, a 5-halosubstituted uracil base, exhibit unexpectedly high activity against Epstein-Barr virus (EBV), Varciella-Zoster virus (VZV) and Herpes Virus 8 (HV-8). In particular, the compounds according to the present invention show potent inhibition of the replication of the virus (viral growth) in combination with very low toxicity to the host cells (i.e., animal or human tissue). Compounds are useful for treating EBV, VZV and HV-8 infections in humans.
Claims
exact text as granted — not AI-modifiedWe claim:
1. A method for treating a viral infection in a patient caused by Varicella-Zoster virus or comprising administering to said patient a therapeutically effective amount of a compound according to the structure: ##STR6## where R is Br or I, and R 1 is H, a C 1 to C 20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group.
2. The method according to claim 1 wherein R 1 is H, a C 1 to C 20 acyl group, a phosphate group or a phosphodiester group.
3. The method according to claim 2 wherein R is I.
4. The method according to claim 2 wherein R is Br.
5. The method according to claim 1 where R 1 is a C 1 to C 3 acyl group.
6. The method according to claim 1 where R is or I.
7. A method for treating a Varicella-Zoster virus infection in a patient comprising administering to said patient a therapeutically effective amount of a compound according to the structure: ##STR7## where R is Br or I and R 1 is H.
8. The method according to claim 7 where R is Br.
9. The method according to claim 7 where R is I.
10. A method for preventing or delaying the onset of EBV-related lymphoma or cancer or Kaposi's Sarcoma in EBV-infected patients comprising administering to said patent at risk for an EBV-related lymphoma or cancer a therapeutically effective amount of a compound according to the formula: ##STR8## where R is Br or I; and R 1 is H, a C 1 to C 20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group.
11. The method according to claim 10 wherein R 1 is H and R is Br.
12. The method according to claim 10 wherein said patient is immunodeficient.
13. The method according to claim 10 wherein said patient is an organ transplant patient.
14. The method according to claim 10 wherein said patient has had a blood transfusion.
15. The method according to claim 10 wherein R is I.
16. The method according to claim 10 wherein R 1 is H, a C 1 to C 20 acyl group, a phosphate group or a phosphodiester group.
17. The method according to claim 16 wherein R is I.
18. The method according to claim 16 wherein R is Br.
19. The method according to claim 10 wherein R 1 is H and R is I.
20. A method for treating a virus infection in a patient caused by Kaposi's Sarcoma virus (HV-8) comprising administering to said patient a therapeutically effective amount of a compound according to the structure: ##STR9## where R is Br or I and R 1 is H, a C 1 to C 20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group.
21. The method according to claim 20 where R is Br or and R 1 is H.
22. The method according to claim 21 where R is Br.
23. The method according to claim 21 where R is I.
24. The method according to claim 20 wherein R 1 is H, a C 1 to C 20 acyl group, a phosphate group or a phosphodiester group.
25. The method according to claim 24 wherein R is I.
26. The method according to claim 24 wherein R is Br.
27. A method for preventing or delaying the onset of Kaposi's Sarcoma in a HIV-infected patient comprising administering to said patient a therapeutically effective amount of a compound according to the formula: ##STR10## where R is Br or I and R 1 is H, a C 1 to C 20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group.
28. The method according to claim 27 wherein R 1 is H and R is I or Br.
29. The method according to claim 28 wherein R is Br.
30. The method according to claim 27 wherein said patient is immunodeficient.
31. The method according to claim 27 wherein said patient is an organ transplant patient.
32. The method according to claim 27 wherein said patient has had a blood transfusion.
33. The method according to claim 28 wherein R is I.
34. The method according to claim 27 wherein R 1 is H, a C 1 to C 20 acyl group, a phosphate group or a phosphodiester group.
35. The method according to claim 34 wherein R is I.
36. The method according to claim 34 wherein R is Br.
37. A method of treating an Epstein-Barr virus infection in a patient comprising administering to said patient a therapeutically effective amount of a compound according to the structure: ##STR11## where R is Br or I and R 1 is H, a C 1 to C 20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group.
38. The method according to claim 37 wherein R 1 is H, a C 1 to C 20 acyl group, a phosphate group or a phosphodiester group.
39. The method according to claim 38 wherein R is I.
40. The method according to claim 37 wherein R is Br.
41. The method according to claim 37 wherein R is I.
42. The method according to claim 38 wherein R is Br.Cited by (0)
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